human glucagon receptor

Semaglutide is a glucagon-like peptide 1 receptor (GLP-1R) agonist(EC50 of 6.2 pM in a reporter assay using BHK cells expressing the human receptor).

GLP-1R Agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).

GRA Ex-25 (GRA-Ex-25) is an inhibitor of glucagon receptor.

GLP-1 secretion by human enteroendocrine NCI-H716 cells is augmented in a dose-dependent manner by the addition of CPE.

Glucagon (1-29), bovine, human, porcine is a hormone produced by pancreatic α-cells with glucagon activity, which promotes glycogenolysis and gluconeogenesis, and is used in the study of obesity and diabetes.

Glucagon (1-29), bovine, human, porcine hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone produced by pancreatic α-cells that activates HNF4α, increases HNF4α phosphorylation, and stimulates gluconeogenesis.

ECC5004 is a compound that activates the glucagon-like peptide-1 receptor (GLP-1R). In HEK293 cells expressing the human GLP-1R, ECC5004 induces cAMP accumulation with an EC50 value of less than 20 nM.

L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.

Skyrin is a fungal metabolite characterized by a bisanthraquinone structure. It interferes with glucagon signaling through adenylate cyclase without binding to the glucagon receptor. At 10 μM, skyrin reduces both glucagon-stimulated cAMP production and glycogenolysis. It does not interfere with epinephrine or glucagon-like peptide 1 effects on these parameters.[1] Reference:[1]. Parker, J.C., McPherson, R.K., Andrews, K.M., et al. Effects of skyrin, a receptor-selective glucagon antagonist, in rat and human hepatocytes. Diabetes 49, 2079-2086 (2012).

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

Glucagon receptor antagonist I is a competitive antagonist of the glucagon receptor (GCGR; IC50 = 181 nM). It blocks glucagon-induced glycogenolysis in primary human hepatocytes and isolated liver. Glucagon receptor antagonist I, at 50 mg/kg, reduces the increase in glucose levels observed after intraperitoneal administration of glucagon in humanized mice. Glucagon receptor antagonist inactive control does not prevent glucagon-mediated actions.

GCGR Antagonist 2, a Furan-2-carbohydrazide, serves as an orally active antagonist of the glucagon receptor. It exhibits affinity for the human glucagon receptor (hGluR) with a dissociation constant (Kd) of 2.3 nM and demonstrates inhibitory activity against the rat receptor with a half-maximal inhibitory concentration (IC50) of 0.43 nM. Additionally, this compound effectively prevents glucagon-stimulated glycogenolysis.

NNC-0640 is a negative allosteric modulator of Human Glucagon Receptor with an IC50 of 69.2 nM.

Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist. Albiglutide TFA significantly reduces glycosylated hemoglobin (A1C). Albiglutide TFA can be used for type 2 diabetes (T2D) research. Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin [1] [2] [3] .

GLP-1(9-36)amide TFA, a predominant metabolite of glucagon-like peptide-1-(7-36)amide synthesized through dipeptidyl peptidase-4 (DPP-4) activity, functions as an antagonist to the human pancreatic GLP-1 receptor [1] [2].

Retatrutide acetate (LY3437943) is a peptide and triple agonist for the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R), exhibiting potent inhibitory effects on human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM respectively; it is utilized in obesity research [1].

Gulgafafusp alfa is a human IgG2κ monoclonal antibody that selectively binds to the glucagon-like peptide 1 receptor (GLP1R) [1].

Tirzepatide acts as an agonist for both the glucagon-like peptide 1 receptor (GLP-1R) and G protein-coupled receptor 119 (GPR119), effectively inducing cAMP production in HEK293 cells that express either human GLP-1R or GPR119, with EC50 values of 6.54 and 1.01 nM, respectively. Additionally, at a concentration of 100 nM, it triggers receptor internalization in these cells. In vivo studies demonstrate that tirzepatide, administered at 10 nmol/kg per day, significantly reduces body weight, food intake, as well as plasma and hepatic triglyceride levels, free fatty acids (FFAs), leptin, and blood glucose in mice with high-fat diet-induced obesity. Furthermore, a dose of 50 nmol/kg every three days prevents an increase in eosinophils and lymphocytes in the bronchoalveolar lavage fluid (BALF) and inhibits bronchoconstriction prompted by methacholine in mice models of both asthma and diabetes, indicating its potential in treating type 2 diabetes mellitus.

5(S)-HEPE, an active metabolite of eicosapentaenoic acid (EPA), is produced via the action of 5-lipoxygenase (5-LO). This compound functions as an agonist for G protein-coupled receptor 119 (GPR119), promoting cAMP accumulation in CHO-K1 cells expressing human GPR119 at 10 µM concentration. Additionally, 5(S)-HEPE enhances glucose-stimulated insulin secretion from MING6 insulinoma pancreatic islets and glucagon-like peptide 1 (GLP-1) secretion from HuTu 80 adenocarcinoma cells at the same concentration. Notably, serum levels of 5(S)-HEPE are increased in hyperlipidemia patients.

Glucagon-like peptide 1 (1-37), human (TFA), is a highly potent agonist of the GLP-1 receptor and is a pancreatic hormone synthesized through post-translational processing of proglucagon.

Glucagon-like peptide 1 (1-37), human, is a highly potent agonist of the GLP-1 receptor and a pancreatic hormone synthesized by post-translational processing of proglucagon. Unlike truncated forms of GLP-1, it neither affects food intake in rats nor enhances pancreatic insulin secretion.

Glucagon-like peptide 1 (1-37), human acetate is a highly potent the GLP-1 receptor agonist.

Glucagon (19-29), human acetate a COOH-terminal fragment processed from glucagon, is a potent and efficient inhibitor of insulin secretion.